反应详情

To 10 mmol of (S)-N2-(benzyloxycarbonyl)-arginine suspended in a mixture of acetone/water 80/20 there is added, at 0° C., a sufficient amount of 4N sodium hydroxide solution to bring the pH of the reaction mixture to between 11 and 11.5. After stirring for 2 hours, there is then added a solution of methanesulphonyl chloride in acetone and then, after stirring for a further 3 hours, the mixture is neutralised using 1N hydrochloric acid solution; the acetone is then evaporated off, and the residue obtained is extracted with ether and then washed, dried, filtered and evaporated. The pale yellow oil thereby obtained is purified by chromatography over silica (eluant: dichloromethane/methanol 7/3) to yield the expected product in the form of a whitish meringue.

1. additionis added, at 0° C.
2. stirringafter stirring for a further 3 hours
3. customthe acetone is then evaporated off
4. customthe residue obtained
5. extractionis extracted with ether
6. washwashed
7. customdried
8. filtrationfiltered
9. customevaporated
10. customThe pale yellow oil thereby obtained
11. customis purified by chromatography over silica (eluant: dichloromethane/methanol 7/3)